PF 06551600 malonate

Name: PF 06551600 malonate
Brand: Tocris Bioscience
SKU: 6506
Rating: 5 (1 reviews)

Tocris Bioscience, part of Bio-Techne | Catalog # 6506

(1)

Citations (4)

COA / SDS

Potent and selective JAK3 inhibitor

Key Product Details

Description:	Potent and selective JAK3 inhibitor
Chemical Name:	1-[(2S,5R)-2-Methyl-5-(7H-pyrrolo[2,3-d]pyrimidin-4-ylamino)-1-piperidinyl]-2-propen-1-one malate
Purity:	≥98% (HPLC)
Molecular Weight:	389.41

View Full Technical Details for PF 06551600 malonate

Technical Data
Citations / Reviews (1)

Biological Activity for PF 06551600 malonate

PF 06551600 malonate is a potent and selective JAK3 inhibitor (IC₅₀ = 33.1 μM). Exhibits no significant activity against a panel of other kinases including JAK1, JAK2 and TYK2. Inhibits phosphorylation of STAT5, induced by IL-2, IL-4, IL-7 and IL-15. Suppresses Th1 and Th17 T-cell differentiation and function in vitro. Reduces paw swelling in a rat model of arthritis and reduces disease severity in a rat EAE model.

Licensing Information

Sold for research purposes under agreement from Pfizer Inc.

Compound Libraries for PF 06551600 malonate

PF 06551600 malonate is also offered as part of the Tocriscreen 2.0 Max and Tocriscreen Epigenetics Library. Find out more about compound libraries available from Tocris.

Technical Data for PF 06551600 malonate

M. Wt	389.41
Formula	C₁₅H₁₉N₅O.C₃H₄O₄
Storage	Store at +4°C
Purity	≥98% (HPLC)
CAS Number	2140301-97-7
PubChem ID	124203830
InChi Key	QMPMPSGDPRHZCG-VZXYPILPSA-N
Smiles	C[C@H]1CC[C@@H](NC2=C3C=CNC3=NC=N2)CN1C(C=C)=O.OC(CC(O)=O)=O

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

Tocris products are intended for laboratory research use only, unless stated otherwise.

Solubility for PF 06551600 malonate

	Solvent	Max Conc. mg/mL	Max Conc. mM
Solubility
	water	38.94	100
	DMSO	38.94	100

Preparing Stock Solutions for PF 06551600 malonate

The following data is based on the product molecular weight 389.41.

Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
1 mM	2.57 mL	12.84 mL	25.68 mL
5 mM	0.51 mL	2.57 mL	5.14 mL
10 mM	0.26 mL	1.28 mL	2.57 mL
50 mM	0.05 mL	0.26 mL	0.51 mL

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Reconstitution Calculator

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References for PF 06551600 malonate

References are publications that support the biological activity of the product.

Telliez Discovery of a JAK3-selective inhibitor: functional differentiation of JAK3-selective inhibition over pan-JAK or JAK1-selective inhibition. ACS Chem.Biol. 2016 PMID: 27791347
Thorarensen Design of a Janus Kinase 3 (JAK3) specific inhibitor 1-((2S,5R)-5-((7H-pyrrolo[2,3-d]pyrimidin-4-yl)amino)-2-methylpiperidin-1-yl)prop-2-en-1-one (PF-06651600) allowing for the interrogation of JAK3 signaling in humans. J.Med.Chem. 2017 PMID: 28139931